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1.
Socrates C. H. Cavalcanti Yuejun Xiang M. Gary Newton Raymond F. Schinazi Yung-Chi Cheng Chung K. Chu 《Nucleosides, nucleotides & nucleic acids》2013,32(10):2233-2252
Abstract A series of 2′,3′-dideoxy-2′-fluoro-L-threo-pentofuranosyl nucleosides has been synthesized as potential antiviral agents. The synthesized compounds were evaluated against HIV-1, HBV, HSV-1, and HSV-2. Among the synthesized analogues, only the cytosine derivative showed moderate antiviral activity against HIV and HBV. 相似文献
2.
Pierra C Olgen S Cavalcanti SC Cheng YC Schinazi RF Chu CK 《Nucleosides, nucleotides & nucleic acids》2000,19(1-2):253-268
Cyclopropyl carbocyclic nucleosides have been synthesized from the key intermediate 2 which was converted to the mesylated cyclopropyl methyl alcohol 3. Condensation of compound 3 with various purine and pyrimidine bases gave the desired nucleosides. All synthesized nucleosides were evaluated for antiviral activity and cellular toxicity. Among them adenine 22 and guanine 23 derivatives showed moderate antiviral activity against HIV-1 and HBV. None of the other compounds showed any significant antiviral activities against HIV-1, HBV, HSV-1 and HSV-2 in vitro up to 100 microM. 相似文献
3.
Cavalcanti SC Xiang Y Newton MG Schinazi RF Cheng YC Chu CK 《Nucleosides & nucleotides》1999,18(10):2233-2252
A series of 2',3'-dideoxy-2'-fluoro-L-threo-pentofuranosyl nucleosides has been synthesized as potential antiviral agents. The synthesized compounds were evaluated against HIV-1, HBV, HSV-1, and HSV-2. Among the synthesized analogues, only the cytosine derivative showed moderate antiviral activity against HIV and HBV. 相似文献
4.
Abstract Geminal difluorocyclopropane analogues of nucleosides 7a–7e were synthesized. Compounds 7a and 7c–7e were obtained by alkylation of nucleic acid bases or their appropriate precursors with (cis)-1-benzyloxymethyl-2-bromomethyl-3,3-difluorocyclopropane (8). Analogue 7b was prepared by hydrolysis of 2-amino-6-chloropurine derivative 7e. Compounds 7a–7d did not exhibit any antiviral activity against HCMV, HSV-1, HSV-2, EBV, VZV, HBV and HIV-1 or antitumor effects against murine leukemia L1210, mouse tumors PO3 or C38 and human tumor H15. 相似文献
5.
Naina A. Van Draanen George W. Koszalka 《Nucleosides, nucleotides & nucleic acids》2013,32(8):1679-1693
Abstract A series of α-L-2′,3′-dideoxy nucleosides was prepared as potential antiviral agents. The pyrimidine nucleosides were prepared by standard Vorbrüggen coupling reactions. The purine analogues were prepared by enzymatic transfer of the dideoxy sugar from a pyrimidine to a purine base. These compounds were inactive against HIV-1, HBV, HSV-1 and -2, VZV, and HCMV. 相似文献
6.
A series of 2'-deoxyapio-L-furanosyl pyrimidine nucleosides were efficiently synthesized starting from D-lactose via condensation of lactitor acetates with silylated pyrimidine bases under standard Vorbrüggen conditions. Their structures were determined by 1D and 2D NMR spectroscopy. All the synthesized nucleosides were assayed against several viruses such as HIV-1, HBV, HSV-1, HSV-2, and HCMV. However, none of these compounds had any significant antiviral activity at concentrations up to 100 microM. 相似文献
7.
Yao-Ling Qiu Mohamad B. Ksebati Jiri Zemlicka 《Nucleosides, nucleotides & nucleic acids》2013,32(1-2):31-37
Abstract Synthesis of Z- and E-methylenecyclopropane analogues of adenosine 3 and 4 by alkylation of adenine with novel alkylating agent 5 is described. The E-isomer 4 is a substrate for adenosine deaminase. Compounds 3 and 4 were tested for antiviral activity against HCMV, HSV-1, HSV-2, EBV, VZV, HBV and HIV-1. 相似文献
8.
9.
Joon Hee Hong So-Young Kim Chang-Hyun Oh Kyung Ho Yoo Jung-Hyuck Cho Prof. Dr. 《Nucleosides, nucleotides & nucleic acids》2013,32(3):341-350
Novel acyclic nucleoside analogues were designed and synthesized as open-chain analogues of neplanocin A. The coupling of the allylic bromide with purine bases using cesium carbonate afforded a series of novel acyclic nucleosides. The synthesized compounds Ia – II were evaluated for their antiviral activity against various viruses such as HIV, HSV-1, HSV-2, and ECMV. 相似文献
10.
Lak Shin Jeong Hyung Ryong Moon Su Jeong Yoo Sun Nan Lee Hee-Doo Kim Moon Woo Chun 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):571-572
Abstract L-2′-Deoxy-2′-up-fluoro-4′-thionucleosides were efficiently synthesized from D-xylose via L-4-thioarabitol derivative as a key intermediate and evaluated for antiviral activities against HIV-1, HSV-1,2 and HBV. 相似文献
11.
In these study, novel acyclic (E)-bromovinyl nucleosides were synthesized as potential antiviral agents. The coupling of the allylic bromide 9 with bases (thymine, uracil, 5-fluorouracil, 5-iodouracil, cytosine, adenine) afforded a series of novel acyclic nucleosides. The synthesized compounds were evaluated for their antiviral activity against various viruses such as HIV-1, HSV-1, HSV-2, and HCMV. 5-Iodouracil analogue 19 showed weak anti-HIV-1 activity. 相似文献
12.
Lak Shin Jeong Su Jeong Yoo Hyung Ryong Moon Moon Woo Chun Chong-Kyo Lee 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):655-656
Abstract Novel d- and l-isodideoxynucleosides were synthesized starting from d- and l-xylose and evaluated for antiviral activities against HIV-1, HSV-1, HSV-2, HBV and HCMV, respectively. 相似文献
13.
Geminal difluorocyclopropane analogues of nucleosides 7a-7e were synthesized. Compounds 7a and 7c-7e were obtained by alkylation of nucleic acid bases or their appropriate precursors with (cis)-1-benzyloxymethyl-2-bromomethyl-3,3-difluorocyclopropane+ ++ (8). Analogue 7b was prepared by hydrolysis of 2-amino-6-chloropurine derivative 7e. Compounds 7a-7d did not exhibit any antiviral activity against HCMV, HSV-1, HSV-2, EBV, VZV, HBV and HIV-1 or antitumor effects against murine leukemia L1210, mouse tumors PO3 or C38 and human tumor H15. 相似文献
14.
Novel syntheses of 4′-modified cyclopentenyl pyrimidine C-nucleosides were performed via C-C bond formation using SN2 alkylation via the key intermediate mesylates 6 and 16, which were prepared from acyclic ketone derivatives. When antiviral evaluation of synthesized compound was performed against various viruses such as HIV-1, HSV-1 and HSV-2, isocytidine analogue 20 showed moderate anti-HIV activity in CEM cell line (EC50 = 13.1 μmol).7 相似文献
15.
Amalraj Ambrose Jiri Zemlicka Earl R. Kern John C. Drach Elizabeth Gullen Yung-Chi Cheng 《Nucleosides, nucleotides & nucleic acids》2013,32(10-12):1763-1774
The Z- and E-thymine and cytosine pronucleotides 3d, 4d, 3e, and 4e of methylenecyclopropane nucleosides analogues were synthesized, evaluated for their antiviral activity against human cytomegalovirus (HCMV), herpes simplex virus 1 and 2 (HSV-1 and HSV-2), varicella zoster virus (VZV), Epstein-Barr virus (EBV), human immunodeficiency virus type 1 (HSV-1), and hepatitis B virus (HBV) and their potency was compared with the parent compounds 1d, 2d, 1e, and 2e. Prodrugs 3d and 4d were obtained by phosphorylation of parent analogues 1d or 2d with reagent 8. A similar phosphorylation of N4-benzoylcytosine methylenecyclopropanes 9a and 9b gave intermediates 11a and 11b. Deprotection with hydrazine in pyridine–acetic acid gave pronucleotides 3e and 4e. The Z-cytosine analogue 3e was active against HCMV and EBV. The cytosine E-isomer 4e was moderately effective against EBV. 相似文献
16.
Annie-Fransoise Maggio Valerie Boyer Anne-Marie Aubertin Georges Obert André Kirn Jean-Louis Imbach 《Nucleosides, nucleotides & nucleic acids》2013,32(7):1431-1449
Abstract 2′,3′-Secothymidine derivatives related to AZT and ddT have been synthesized and evaluated for their activity against HIV-1 and various DNA and RNA viruses. These acyclic nucleosides exhibited no antiviral activities. 相似文献
17.
《Nucleosides, nucleotides & nucleic acids》2013,32(5-8):845-847
Abstract A series of cyclohexenyl nucleosides (1–8) were successfully prepared with moderate yield and their cytotoxicity and antiviral activity were investigated. Among the eight new compounds, only the diaminopurine analogue 8 showed pronounced activity against HSV-1, HSV-2. 相似文献
18.
Jeong LS Kim YH Kim HO Yoo SJ Park YH Yeon SH Chun MW Kim HD 《Nucleosides, nucleotides & nucleic acids》2001,20(4-7):665-668
Novel D- and L-2'-azido-2',3'-dideoxy-4'-thionucleosides were synthesized starting from L- and D-xylose via D- and L-4-thioarabitol derivative as key intermediates and evaluated for antiviral activity, respectively. When the final nucleosides were tested against HIV-1, HSV-1, HSV-2, and HCMV, they were found to be only active against HCMV without cytotoxicity up to 100 micrograms/ml. 相似文献
19.
Chang Hyun Oh Jin Woo Kim Joon Hee Hong 《Nucleosides, nucleotides & nucleic acids》2013,32(8):871-878
Novel vinyl branched apiosyl nucleosides were synthesized in this study. Apiosyl sugar moiety was constructed by sequential ozonolysis and reductions. The bases (uracil and thymine) were efficiently coupled by glycosyl condensation procedure (persilyated base and TMSOTf). The antiviral activities of the synthesized compounds were evaluated against the HIV-1, HSV-1, HSV-2, and HCMV. Compound 10β displayed moderate anti-HIV activity (EC50 = 17.3 μg/mL) without exhibiting any cytotoxicity up to 100 μM. 相似文献
20.
Palmarisa Franchetti Ghassan Abu Sheikha Paolo Perlini Farhat Farhat Mario Grifantini Graziella Perra 《Nucleosides, nucleotides & nucleic acids》2013,32(10-11):1921-1932
Abstract The synthesis of 9-[2-(phosphonomethoxy)allyl]guanine (1) and 9-[2-(phosphonomethoxy)allyl]-8-aza-guanine (2), two new unsaturated acyclic phosphonate nucleosides analogues of the anti-HIV agents PMPG and 8-aza-PMPG, is described. Compounds 1 and 2 were evaluated for activity against human immunodeficiency virus (HIV-1 and HIV-2) and herpes simplex virus (HSV-1 and HSV-2). 相似文献